Zaleplon

Oral
Insomnia

Debilitated patients: 5 mg immediately before bedtime or after an unsuccessful attempt to fall asleep. Max: 10 mg daily.

Patients taking cimetidine: Initially, 5 mg immediately before bedtime or after an unsuccessful attempt to fall asleep.

Mild to moderate: 5 mg immediately before bedtime or after an unsuccessful attempt to fall asleep. Severe: Not recommended.

May be taken with or without food. Do not take w/ or immediately after a heavy or high fat meal.

Patient who have previous experience of complex sleep behaviours following zaleplon, zolpidem, and eszopiclone therapy. Lactation.

Patient with diseases or conditions that may affect metabolism or haemodynamic responses; signs or symptoms of depression; compromised respiratory function, COPD, sleep apnoea; history of drug or alcohol addiction or dependence. Not recommended for use in severe hepatic impairment. Avoid concomitant use with other sedative and hypnotic drugs. Avoid abrupt withdrawal or rapid dose reduction. Mild to moderate hepatic impairment. Elderly and debilitated patients. Pregnancy.

Significant: Abnormal thinking and behaviour changes (e.g. decreased inhibition, bizarre behaviour, agitation, hallucinations, depersonalisation), amnesia; CNS depression; hypersensitivity reactions (e.g. anaphylaxis, angioedema).
Cardiac disorders: Chest pain.
Ear and labyrinth disorders: Vertigo, otalgia, hyperacusis.
Eye disorders: Eye pain, visual disturbance, conjunctivitis.
Gastrointestinal disorders: Nausea, abdominal pain, constipation, dyspepsia, dysgeusia, xerostomia, colitis.
General disorders and administration site conditions: Fever, asthenia, malaise.
Metabolism and nutrition disorders: Anorexia, peripheral oedema.
Musculoskeletal and connective tissue disorders: Arthralgia, arthritis, back pain, myalgia.
Nervous system disorders: Headache, dizziness, drowsiness, paraesthesia, hypoaesthesia, migraine, hypertonia, tremor.
Psychiatric disorders: Anxiety, depression, nervousness.
Reproductive system and breast disorders: Dysmenorrhoea.
Respiratory, thoracic and mediastinal disorders: Bronchitis, epistaxis.
Skin and subcutaneous tissue disorders: Pruritus, rash, photosensitivity reaction.
Potentially Fatal: Complex sleep behaviours (e.g. sleep walking, sleep driving).

PO: C

This drug may cause drowsiness, dizziness, blurred vision, or reduced alertness the next morning after intake, if affected, do not drive or operate machinery. To minimise these symptoms, get a full night of sleep (7-8 hours) after taking the dose.

Carefully evaluate patient for co-morbidities prior to initiation of treatment. Monitor behaviour changes, respiratory rate (in patient with compromised respiration), daytime alertness. Assess fall risk; history of addiction and risk for suicide. Monitor for tolerance, abuse, and dependence. Re-evaluate if insomnia persists after 30 days of treatment.

Symptoms: Drowsiness, mental confusion, lethargy; ataxia, hypotonia, hypotension, respiratory depression, loss of consciousness. Rarely, coma and very rarely, death. Management: Symptomatic and supportive treatment. Perform gastric lavage if appropriate. Administer IV fluids as necessary. Monitor respiration, pulse, and blood pressure. Monitor and treat patient with appropriate medical intervention in case of CNS depression and hypotension.

May increase plasma concentration and exposure with cimetidine (aldehyde oxidase and CYP3A4 inhibitor) and strong CYP3A4 inhibitors (e.g. erythromycin, ketoconazole). May cause additive CNS effects with other CNS depressants (e.g. imipramine, thioridazine, anaesthetics, anticonvulsants, antihistamines, opiates, other sedatives and hypnotics). May decrease plasma concentration and exposure with CYP3A4 inducers (e.g. rifampicin, phenytoin, carbamazepine, phenobarbital).

Avoid taking with or after a heavy or high-fat meal as absorption may be reduced. May cause additive CNS depressant effect with alcohol.

Description:
Mechanism of Action: Zaleplon, a pyrazolopyrimidine derivative, is a sedative and hypnotic agent that is structurally unrelated to benzodiazepines, barbiturates, or other hypnotics. However, it is found to interact with the GABA-benzodiazepine receptor complex.
Onset: Rapid.
Pharmacokinetics:
Absorption: Rapidly and almost completely absorbed from the gastrointestinal tract. Delayed absorption with or after a heavy or high-fat meal. Bioavailability: Approx 30%. Time to peak plasma concentration: Approx 1 hour.
Distribution: Enters breast milk (small amount). Plasma protein binding: Approx 45-75%.
Metabolism: Extensively metabolised into inactive metabolites, mainly by aldehyde oxidase to form 5-oxo-zaleplon and, to a lesser extent, by CYP3A4 to desethylzaleplon, which is further metabolised to 5-oxo-desethylzaleplon presumably by aldehyde oxidase. Undergoes first-pass hepatic metabolism.
Excretion: Via urine (approx 70% mainly as metabolites, <1% as unchanged drug); faeces (approx 17%, primarily as 5-oxo-zaleplon). Elimination half-life: Approx 1 hour.

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5719, Zaleplon. https://pubchem.ncbi.nlm.nih.gov/compound/Zaleplon. Accessed May 25, 2021.

Store between 20-25°C. Protect from light.

Hypnotics & Sedatives

N05CF03 - zaleplon ; Belongs to the class of benzodiazepine related agents. Used as hypnotics and sedatives.

Anon. Zaleplon. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 23/04/2021.

Anon. Zaleplon. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 23/04/2021.

Buckingham R (ed). Zaleplon. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 23/04/2021.

Zaleplon Capsule (OrchidPharma Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 23/04/2021.